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Solid dispersion and pharmaceutical composition

A solid dispersion and composition technology, applied in the field of medicine, can solve problems such as poor bioavailability, low dissolution rate, and increased side effects of drugs, and achieve the effects of reducing clinical dosage, improving absorption properties, and improving solubility

Pending Publication Date: 2020-11-10
HEFEI COSOURCE PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Compounds with low solubility in water, may have low dissolution rates and thus exhibit poor bioavailability
Compounds with poor bioavailability can pose problems for patient treatment, often due to unpredictability of dosing / therapeutic effects due to erratic absorption of the compound by the patient; for example diet can affect patient absorption as described above for poor bioavailability The ability of the compound to increase the degree, thus may require a dosing regimen that takes into account the effect of food
In addition, due to unpredictable administration effects, the dose may require a large safety margin, and a large dose of the compound may be required to achieve the desired therapeutic effect, which also increases the side effects of the drug
Both formula 1 and formula 2 compounds have the problem of poor bioavailability due to low solubility. In order to improve the solubility of formula 1 and formula 2 compounds in the entire gastrointestinal tract environment, to improve the bioavailability of preparations, poorly soluble drugs are developed It is of great significance to form a pharmaceutical preparation product that exists stably in an amorphous form

Method used

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  • Solid dispersion and pharmaceutical composition
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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] 1) Preparation of solid dispersion 1 of formula 1: add 1 g of compound of formula 1 to 100 mL of 95% ethanol, stir to dissolve to obtain a clear solution, then add 4 g Stir to dissolve; vacuum-dry at 40°C for 24 hours, pass through a 60-mesh sieve to obtain solid dispersion 1 (compound of formula 1+ ).

[0037] 2) Preparation of formula 1 solid dispersion 2: 1g of formula 1 compound is added in 100mL propanol, stirred to dissolve, and a clear solution is obtained; add 0.4g SDS, then add 4g Stir to make it uniform; vacuum-dry at 40°C for 24 hours, and pass through a 60-mesh sieve to obtain solid dispersion 2 (compound of formula 1+ +SDS).

[0038] 3) Formula 1 blend preparation: 1g formula 1 compound, 0.4g SDS, 4g Mix evenly to obtain a physical mixture (blend of formula 1).

Embodiment 2

[0040] Add 1g of the compound of formula 1 into 100mL of propanol, stir to dissolve, and obtain a clear solution; add 0.4g of SDS, and then add 3g Stir to make it uniform; remove the solvent by fluidized bed spray drying, and pass through a 60-mesh sieve to obtain a solid dispersion.

Embodiment 3

[0042] Add 1g of the compound of formula 1 to 15mL DMA, stir to dissolve, then add 4g HPMCAS, stir to dissolve to obtain an organic phase solution; under high shear conditions, slowly release the organic phase solution into 150ml purified water, filter, 40°C Vacuum-dried for 12 hours, and passed through an 80-mesh sieve to obtain a solid dispersion.

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Abstract

The invention discloses a solid dispersion and a pharmaceutical composition, and relates to the technical field of medicines. The solid dispersion contains an active drug and a carrier material, wherein the active drug is a compound in a formula 1 or formula 2; and the carrier material is any one of hydroxypropyl methylcellulose acetate succinate and hydroxypropyl methylcellulose phthalate. The solid dispersion can improve the solubility and absorption properties of the compound in the formula 1 or formula 2, thereby reducing the clinical dosage. Characterization shows that the compound in theformula 1 or formula 2 is dispersed in the carrier material in an amorphous form and still exists in an amorphous state after being placed for 3 months under an acceleration condition (40 DEG C / 75% RH), and the performance is stable. A preparation prepared from the solid dispersion can greatly reduce the influence of environmental temperature, humidity and the like on product dissolution and bioavailability in the processes of production, transportation, storage and the like of medicines.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a solid dispersion and a pharmaceutical composition. Background technique [0002] N-(4-methyl-3-(1-isonicotinylpiperidin-4-yl)oxy)phenyl)-3-(trifluoromethyl)benzamide (Formula 1) is a R&D A highly selective C-KIT tyrosine kinase inhibitor, which can strongly inhibit the phosphorylation of kinase C-KIT, does not show inhibitory effect on BCR-abl and FLT3 kinases, in the selectivity test of 468 human kinases It shows a small off-target effect and can be used for the treatment of CD117-positive gastrointestinal stromal tumors. The compound of formula 1 has been disclosed in the patent CN107286077A, showing its potentially valuable pharmaceutical properties. [0003] [0004] N-{4-methyl-3-[4-(5-morpholinyl-3-pyridyl)-1H-pyrazol-1-yl]phenyl}-3-trifluoromethyl-benzamide ( Formula 2) is a third-generation Pan-braf kinase small molecule inhibitor under development, which is main...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4545A61K31/5377A61K47/38A61K47/32A61P35/00
CPCA61K31/4545A61K31/5377A61K47/38A61K47/32A61P35/00
Inventor 陈登俊李志云张俊汪贻华吴勇曹杰永
Owner HEFEI COSOURCE PHARMA CO LTD
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